KR840006627A - Method for preparing benzazine derivatives - Google Patents

Abstract

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Description

Method for preparing benzazine derivatives

As this is a public information case, the full text was not included.

Claims (10)

a) oxidizing the benzazine of general formula (II) to ruthenium tetroxide in a solvent, or (b) closing the compound of general formula (III) and optionally converting the compound of general formula (I) Salts, in particular the conversion of physiologically suitable acid addition salts with inorganic or organic acids thereof, to benzazine derivatives of general formula (I) and acid addition salts thereof, in particular How to make. Wherein E represents an ethylene, n-propylene or n-butylene group (optionally substituted by alkyl groups of 1 to 3 carbon atoms); G represents methylene or ethylene group (optionally substituted by an alkyl group having 1 to 3 carbon atoms); R ₁ and R ₂ may be equivalent or different and represent a hydroxy group, alkyl, alkoxy or phenylalkoxy group (in each case the alkyl moiety may contain 1 to 3 carbon atoms), or R ₁ or R ₂ One of which also represents a hydrogen atom, or R ₁ and R ₂ together represent an alkylenedioxy group having 1 to 2 carbon atoms; R ₃ and R ₄ may be the same or different and represent hydrogen or a halogen atom, a hydroxy group, an alkyl or alkoxy group having 1 to R ₄ carbon atoms or a trifluoromethyl or cyano group or one of R ₃ or R ₄ Represents a nitro group or R ₃ and R ₄ together represent an alkylenedioxy group having 1 to 2 carbon atoms and R ₅ represents a hydrogen atom, a hydroxy or amino group, alkyl, alkoxy, alkylamino, dialkyl amino, alkanoylamino Alkoxy carbonylamino or bis (alkoxycarbonyl) amino group (in each case the alkyl moiety may contain from 1 to 3 carbon atoms) or methylamino or ethylamino group substituted with trifluoromethyl group; R ₆ represents a hydrogen atom, alkyl, phenylalkyl, alkanoyl or alkoxycarbonyl group (in each case the alkyl moiety may contain 1 to 3 carbon atoms) or an alkenyl group of 3 to 5 carbon atoms; R ₆ ′ represents a protecting group of an amino group or R ₆ described above; X represents a group suitable for ring closure. The process of claim 1, wherein the ruthenium tetroxide used for oxidation is prepared in the reaction mixture. The process according to claim 1 a) or 2, wherein the oxidation reaction is carried out at a temperature between 0 and 100 ° C, preferably between 20 and 50 ° C. The process according to claim 1, wherein the reaction is carried out at 100 to 250 ° C, preferably at 140 to 180 ° C. The process of claim 1 b) or 4, wherein the reaction is carried out in a solvent. The process of claim 1 b), 4 or 5, wherein the reaction is carried out in the presence of a condensing agent. Process according to claim 1 b) or 4 to 6, wherein OH and NH ₂ groups, when present, are protected during the reaction and removed after the reaction. 7. N, N'-dicyclo-hexylcarbodiimide or thionylchloride, phosphonate, phosphoran or N-alkyl-pyridinium salt, N, N'-dicyclohexyl carbodiimide / N, N'-carbonyldiimidazole is also used as a condensing agent when 4-dimethylaminopyridine, chlorosulfonyl isocyanate, or R ₆ is not a hydrogen atom. 8. The method of claim 7, wherein an acyl group is used as a protecting group, which group is removed by hydrolysis after the reaction. 8. A process according to claim 7, wherein a benzyl group is used as the protecting group, which group is removed by hydrogenation after the reaction. ※ Note: It is to be disclosed based on the initial application.